STEROID CONTAINING DRUG DELIVERY SYSTEMS

• US 20090082321A1
• Filed: 09/21/2007
• Published: 03/26/2009
• Est. Priority Date: 09/21/2007
• Status: Abandoned Application

• Current Assignee: Allergan, Inc. (Canada) (Abbvie Incorporated)
• Original Assignee: Allergan, Inc. (Canada) (Abbvie Incorporated)
• Inventors: EDELMAN, JEFFREY L., Harrison, Kelly M., Hughes, Patrick M., Spada, Lon T.
• Application Number:
  US11/859,627
• Publication Number:
  US 20090082321A1
• Time in Patent Office: Days
• US Class Current: 514/178
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• CPC Class Codes: A61K 47/36 Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61K 9/0051 Ocular inserts, ocular implants
• CPC Class Codes: A61K 9/06 Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels composition of ointments, creams or gels A61K47/00
• CPC Class Codes: A61P 27/02 Ophthalmic agents

Abstract

Pharmaceutical composition for intraocular use comprising a glucocorticoid derivative, such as beclomethasone 17,21-diproprionate admixed with a biodegradable polymer such as a poly(lactide-co-glycolide) polymer or a high molecular weight polymeric hyaluronic acid are disclosed.

Claims

1. A solid ophthalmic composition comprising:

(a) a Glucocorticoid Derivative (GD) having a structure effective to prevent diffusion of a biologically significant amount of the GD to the anterior chamber when the GD is administered to the posterior chamber of the eye, and

(b) a biodegradable polymer, wherein therapeutic amounts of the GD is released from the polymer in vitro in a linear release rate.

2. The composition of claim 1, wherein linear release rate persists for at least about 50 days.

3. The composition of claim 1 wherein said GD has a lipophilicity greater than 2.53.

4. The composition of claim 1 wherein said GD has an aqueous solubility less than 10 μ

g/ml.

5. The composition of claim 1, wherein the GD is selected from the group consisting of dexamethasone 17-acetate, dexamethasone 17,21-acetate, dexamethasone 21-acetate, clobetasone 17-butyrate, beclomethasone 17,21-dipropionate (BDP), fluticasone 17-propionate, clobetasol 17-propionate, betamethasone 17,21-dipropionate, alclometasone 17,21-dipropionate, dexamethasone 17,21-dipropionate, dexamethasone 17-propionate, halobetasol 17-propionate, and betamethasone 17-valerate, and salts, esters and derivatives and combinations thereof.

6. The composition of claim 1 wherein the biodegradable polymer is selected from the group consisting of poly (lactide-co-glycolide) polymer (PLGA), poly-lactic acid (PLA), poly-glycolic acid (PGA), polyesters, poly (ortho ester), poly(phosphazine), poly (phosphate ester), polycaprolactones, gelatin, and collagen, and derivatives and combinations thereof.

7. An ophthalmic composition comprising:

(a) beclomethasone 17,21-dipropionate dipropionate (BDP), and

(b) poly(lactide-co-glycolide) polymer (PLGA).

8. A viscous ophthalmic composition comprising:

(a) a Glucocorticoid Derivative (GD) having a structure effective to prevent diffusion of a biologically significant amount of the GD to the anterior chamber when the GD is administered to the posterior chamber of the eye, and

(b) a biodegradable viscosity inducing component.

9. The composition of claim 8, wherein the GD is selected from the group consisting of dexamethasone 17-acetate, dexamethasone 17,21-acetate, dexamethasone 21-acetate, clobetasone 17-butyrate, beclomethasone 17,21-dipropionate (BDP), fluticasone 17-propionate, clobetasol 17-propionate, betamethasone 17,21-dipropionate, alclometasone 17,21-dipropionate, dexamethasone 17,21-dipropionate, dexamethasone 17-propionate, halobetasol 17-propionate, and betamethasone 17-valerate, and salts, esters and derivatives and combinations thereof.

10. The composition of claim 8 wherein the biodegradable viscosity inducing component is a hyaluronic acid or sodium hyaluronate.

11. A viscous ophthalmic composition comprising beclomethasone 17,21-dipropionate (BDP) and a hyaluronic acid or sodium hyaluronate.

12. A method of treating an ocular condition, the method comprising the step of administering to the posterior segment of an eye an ophthalmic composition comprising beclomethasone 17,21-dipropionate dipropionate (BDP) mixed with either a poly(lactide-co-glycolide) polymer (PLGA) or a hyaluronic acid.